BIBU 1361 dihydrochloride

Catalog #: 2417 Datasheet / COA / SDS

Discontinued Product

2417 has been discontinued.
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BIBU 1361 dihydrochloride | CAS No. 1643609-75-9 | EGF Receptor Inhibitors
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Description: Selective inhibitor of EGFR-kinase

Chemical Name: N-(3-Chloro-4-fluorophenyl)-6-[4-[(diethylamino)methyl]-1-piperidinyl]-pyrimido[5,4-d]pyrimidin-4-amine dihydrochloride

Purity: ≥97%

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Biological Activity

BIBU 1361 dihydrochloride is a potent inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase (IC50 = 3 nM). Displays ~ 100-fold lower potency against ErbB2 (IC50 = 290 nM) and is selective over a range of other related tyrosine kinases (IC50 > 10 μM). Blocks downstream EGFR signaling events such as MAPKK/MAPK activation. Oral administration inhibits growth of established human xenografts in athymic mice.

Technical Data

M.Wt:
516.87
Formula:
C22H27ClFN7.2HCl
Solubility:
Soluble to 100 mM in water and to 25 mM in DMSO
Purity:
≥97%
Storage:
Desiccate at +4°C
CAS No:
1643609-75-9

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Inhibition of epidermal growth factor receptor activity by two pyrimidopyrimidine derivatives.
    Solca et al.
    J.Pharmacol.Exp.Ther., 2004;311:502

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